Design, Synthesis of Novel Cyclic Pentapeptide Derivatives Based on 1,2-Benzenedicarbonyl Chloride with Expected Anticancer Activity
Linear pentapeptide ester, phthaloyl-bis-[glycylglycine]-OMe, 3, have been prepared via coupling of N-phthalic acid or dichloride with glycylglycine ester, which was hydrolyzed to the corresponding acid, phthaloyl-bis-[glycylglycine], 4. Cyclization of tetrapeptide acids to give cyclic pentapeptide esters, acids and hydrazides. A preliminary cytotoxicity evaluation (National Cancer Institute, Cairo, EGYPT), for a representative example, Cyclo-(phthaloyl)-)-bis-[glycylglycine]-L-Lys-OMe (phthaloyl cyclic pentapeptide methyl ester) 5, against ... Read more